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Compound Detail

CHEMBL52989

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CCO/C(O)=C1\C(COCCn2cc(C(N)=O)nn2)=NC(C)=C(C(=O)OC)C1c1ccccc1Cl

Basic Information

ChEMBL ID CHEMBL52989
Phase Preclinical
Structure Type MOL
InChI Key CCVXIFHZZOGTQS-BSYVCWPDSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

503.9
MW (Da)
2.54
ALogP
10
HBA
2
HBD
151.2
PSA (Ų)
0.28
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H26ClN5O6
MW 503.94
Aromatic Rings 2
Heavy Atoms 35
NP-Likeness -1.50

Activity Summary

IC50 1 meas. best 7.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Rattus norvegicus
CHEMBL376
IC50 7.7 7.7 19.9 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Rattus norvegicus IC50 = 19.95 nM 7.7 Concentration required to block Ca+2-induced contraction of K+ depolarized rat a... 2342074

Literature References

PubMed DOI Target Context # Activities
2342074 10.1021/jm00168a041 Rattus norvegicus 1
2342074 10.1021/jm00168a041 Cavia porcellus 1
2342074 10.1021/jm00168a041 Unchecked 1

Data from ChEMBL 36 via Core Engine